Inhibitors Against SARS-CoV-2

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PLpro Inhibitors Against SARS-CoV-2 Tech ID: UA21-133 Invention: There are two cysteine proteases that are encoded by SARS-CoV-2, the main protease (Mpro) and the papain-like protease (PLpro). Both of these proteases have been shown to be essential in viral replication and are validated antiviral drug targets. PLpro cleaves the viral SARS-CoV-2 polyprotein at three sites. In addition, it modulates host immune response by cleaving the ubiquitin and ISG modifications from host proteins. This technology identified several novel compounds that are effective in inhibiting SARS-CoV-2 PLpro. Because of its role in viral replication and immune modulating, inhibition of PLpro is expected to provide therapeutic benefits in patients that are infected with SARS-CoV-2. Background: As of February 1, 2021, there have been over 27 million cases of SARS-CoV-2 in the United States and nearly half a million deaths related to the virus. Worldwide there have been over 100 million cases of COVID-19, with over 2.2 million dead from the virus. The virus also has been damaging to the global economy as well as the U.S. economy. Despite the devastation caused by the virus, there are still very few FDA-approved treatments for those who become infected with the virus. In late 2020, two vaccines were approved for emergency use to be administered to prevent the disease; however, a very small percentage of individuals have been able to receive that vaccine. Therefore, it is essential that more treatment options become available for those that become ill with COVID-19. This technology introduces novel, highly-potent PLpro inhibitory compounds that will be able to be used to stop the viral replication of COVID-19. This can be used retroactively to slow the spread of the disease in individuals who have already become infected with COVID-19. PLpro inhibitors have also been shown to be useful antivirals for other human coronaviruses, giving this technology potential to be used to develop treatments for future infectious diseases that resemble COVID-19.